phosphodiesterase inhibitors Flashcards

1
Q

selective inhibition of PDE 3 decreases the breakdown of what?

A

cAMP

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2
Q

increased cAMP in the myocardium stimulates what to phosphorylate the SR?

A

protein kinases

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3
Q

the phosphorylated SR causes an increased influx of what?

A

Ca

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4
Q

increased Ca leads to an increase or decrease in myocardial contractility?

A

increase

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5
Q

increased cAMP in vascular SM increases or decreases available Ca?

A

decreases

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6
Q

increased cAMP in vascular SM decreases available Ca by facilitating the uptake of Ca by what?

A

SR

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7
Q

this uptake of Ca into the vascular SM’s SR causes the SM to do what and the vessels to do what?

A

relax, dilate

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8
Q

do selective PDE 3 inhibitors relax SM in the arteries, veins or both?

A

both

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9
Q

what is the combined effect of PDE 3 inhibitors?

A

positive inotrope with vascular SM relaxation

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10
Q

Do PDE 3 inhibitors increase or decrease these physiologic effects?

  1. contractility
  2. CO
  3. LVEDP
  4. venous capacity
  5. filling pressures (CVP, PCWP)
  6. venous return to the heart
  7. mean PAP
  8. pulmonary vascular resistance
  9. SVR
A
  1. increase
  2. increase
  3. decrease
  4. increase
  5. decrease
  6. decrease
  7. decrease
  8. decrease
  9. decrease
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11
Q

Amrinone has dose-dependent positive inotropic and vasodilator effects that increases what physiologic effect and decreases what physiologic effect?

A

CO, LVEDP

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12
Q

large fraction of Amrinone undergoes what 2 liver elimination processes? (NA, G)

A

N-acetylation and glucuronidation

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13
Q

what is the loading dose of Amrinone (mg/kg) and what is the maintenance infusion rate (mcg/kg/min)?

A

0.5-1.5 mg/kg; 2-10 mcg/kg/min

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14
Q

what are 3 SEs of Amrinone? (one with rapid infusion, one dose-related, one d/t increased myocardial Ca)

A

hypotension, thrombocytopenia, cardiac arrythmias

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15
Q

Amrinone causes dose-related thrombocytopenia by increasing cAMP in plts, which inhibits what sequence at several steps? (PAS)

A

plt activation sequence

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16
Q

milrinone is how many times more potent as an inotrope than amrinone?

A

30 times

17
Q

in what 2 ways does milrinone improve CO?

A

increases inotropy, relaxes vascular SM

18
Q

what is milrinone bolus dose (mcg/kg) given over how many minutes, which is followed by a continuous infusion of what rate (mcg/kg/min)?

A

50 mcg/kg over 10 minutes; 0.375-0.75 mcg/kg/min

19
Q

what percent of milrinone is protein bound?

A

70%

20
Q

what percent of milrinone is excreted unchanged by the kidneys?

A

80%

21
Q

milrinone dose needs to be decreased in pts with what?

A

renal impairment

22
Q

milrinone is useful in managing acute dysfunction of what such as after cardiac surgery?

A

acute LV dysfunction

23
Q

milrinone enhances the weaning from what?

A

cardio-pulmonary bypass

24
Q

milrinone can also be used as a bridge to what? (OHT)

A

orthotopic heart transplant

25
Q

milrinone may potentiate the effects of what type of agents?

A

adrenergic agents

26
Q

milrinone may help increase inotropy in what pts who have down regulations of beta 1 receptors?

A

chronic HF

27
Q

is milrinone or dobutamine more useful and more effective at treating pulmonary HTN by decreasing PAPs?

A

milrinone

28
Q

inotropic effects of milrinone are decreased in what setting?

A

acidosis

29
Q

why is milrinone’s inotropic effects decreased in acidotic muscle?

A

decreased cAMP formation in acidotic muscle

30
Q

what are 2 SEs of milrinone? (H, P)

A

hypotension, proarrythmic

31
Q

what 2 types of arrhythmias have been reported with milrinone?

A

ventricular and supraventricular

32
Q

what automaticity may be increased by milrinone in ischemic myocardium?

A

ventricular automaticity

33
Q

does milrinone or amrinone have more effects on plts?

A

amrinone